title: Inhibitory actions of desacetylation products of phenacetin and paracetamol on prostaglandin synthetases in neuronal and glial cell lines and rat renal medulla.
abstract: The inhibitory actions of phenacetin and paracetamol and of their desacetylation products on prostaglandin synthesis were studied on enzyme preparations originating from a neuronal cell line (mouse neuroblastoma, clone N2A), a glial cell line (rat astrocytoma, clone C6) and rat renal medulla. All compounds tested inhibited cultured cell and kidney prostaglandin synthetases to similar extents. p-Phenetidine and p-aminophenol, the desacetylated metabolites of phenacetin and paracetamol, were either 7-10 times or 4 times more potent than paracetamol. Thus, p-Phenetidine inhibited prostaglandin synthesis as efficaciously as did acetylsalicylic acid. The possible roles of p-phenetidine as the active metabolite of phenacetin for cyclo-oxygenase inhibition in brain and of phenacetin as an organ pro-drug are discussed.
mesh_terms: D000082:Acetaminophen / Q000494:pharmacology*; D000627:Aminophenols / Q000494:pharmacology*; D000818:Animals; D001254:Astrocytoma / Q000201:enzymology; D002460:Cell Line; D016861:Cyclooxygenase Inhibitors; D066298:In Vitro Techniques; D007679:Kidney Medulla / Q000201:enzymology; D008297:Male; D051379:Mice; D009374:Neoplasms, Experimental / Q000201:enzymology; D009447:Neuroblastoma / Q000201:enzymology; D010615:Phenacetin / Q000494:pharmacology*; D010628:Phenetidine / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D000627:Aminophenols; D016861:Cyclooxygenase Inhibitors; D010628:Phenetidine; D000082:Acetaminophen; D010615:Phenacetin; C026729:4-aminophenol